Acquired immune deficiency syndrome (AIDS), which disseminates quickly in the world, has become significant public health event and social hot spot.
AIDS was identified as a disease in 1981 by Centers for Disease Control and Prevention of USA. China experienced its first case of AIDS in 1985. In the past two decades, more and more cases were reported. Nowadays, it has already been spread in many areas of the world. Since China is a country of vast territory and large population, together with the recently frequent international contacts, the number of HIV infections increased year by year. AIDS is a spectrum of conditions caused by the human immunodeficiency virus (HIV), with poor prognosis and high mortality rate. According to the related report of UNAIDS, the population of HIV infections around the world is more than 39 million. Nowadays, India takes over South Africa as the largest population of HIV-infected individuals in the world.
Thus, finding a way to stop the spread of AIDS has become the focus of the world. Most of the Anti-AIDS drugs in clinic are HIV-1 reverse transcriptase inhibitors and HIV-1 protease inhibitors at present time. In humans, the apolipoprotein B mRNA-editing enzyme catalytic polypeptidelike 3G (APOBEC3G, A3G) is a major host-cell factor which can severely weaken the infectivity of HIV-1. It was proved that HIV-1 viral infectivity factor (Vif) can protect the virus from A3G-mediated viral cDNA hypermutation. Therefore, to protect A3 G from degradation, it is very crucial to design inhibitors targeting Vif. In addition, development of multi-target inhibitor of Vif accompanied by other enzymes may improve the therapeutic effect and reduce the virus resistance.
The inventor of this invention endeavored to find the new HIV inhibitors. The inventor has synthesized a series of N-phenyl-2-thiophenylbenzamide derivatives and N-phenyl-2-thiol benzamide derivatives as following:

However, those compounds show general activity, high cytotoxicity, poor solubility and low bioavailability which restrict its application.
In the follow-up project, the inventor found that R1 or R2 substituted by —NH2 or —NH2—R can obviously improve the anti-HIV activity, solubility, druggability and reduce drug toxicity.